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1. 发明专利

IL174860A METHOD FOR PREPARATION OF CRYSTALLINE PERINDOPRIL ERBUMINE 未知
公开(公告)号：IL174860A
公开(公告)日：2011-09-27
申请号：IL17486006
申请日：2006-04-06
申请人： SERVIER LAB , SINGH GIRIJ PAL , GODBOLE HIMANSHU MADHAV , NEHATE SAGAR PURUSHOTTAM , LUPIN LTD
发明人： SINGH GIRIJ PAL , GODBOLE HIMANSHU MADHAV , NEHATE SAGAR PURUSHOTTAM
IPC分类号： C07D209/42

2. 发明申请

WO2012007814A2 THREE COMPONENT CO-CRYSTAL FORMATION BETWEEN DIASTEREOMERIC MIXTURES OF 3-ALKYL-4-((S)-1'PHENYLETHYLAMINO) BUTANOIC ACID AND OPTICALLY PURE 1, 1'-BI-2-NAPHTHOL 审中-公开
标题翻译： 3-烷基-4 - （（S）-1'苯基乙基氨基）丁酸的异构混合物与光学纯的1,1'-BI-2-萘酚之间的三元共晶形成
公开(公告)号：WO2012007814A2
公开(公告)日：2012-01-19
申请号：PCT/IB2011/001605
申请日：2011-07-11
申请人： LUPIN LIMITED , ROY, Bhairab, Nath , SINGH, Girij, Pal , LATHI, Piyush, Suresh , MITRA, Rangan
发明人： ROY, Bhairab, Nath , SINGH, Girij, Pal , LATHI, Piyush, Suresh , MITRA, Rangan
IPC分类号： C07C37/84
CPC分类号： C07C229/14 , C07B2200/07 , C07B2200/13 , C07C37/84 , C07C39/14
摘要： A ternary co-crystal consisting of 1 :0.5:0.5 molar proportion of (S)-1,1'-bi-2-naphthol, 3( S )-propyl-4-[( S )1 '-phenyl-ethylamino]-butanoic acid and 3( R )-propyl-4-[( S )1'- phenyl-ethylamino]-butanoic acid having characteristic powder X-ray diffraction pattern with 2Θ values of 8.41, 9.38, 10.32, 12.16, 15.52, 15.51, 17.84, 17.95, 19.16, 20.37, 21.74, 22.55, 24.44, 25.65, 28.40, 29.15, 29.69, 31.31, 33.54, 34.40, 35.43 (±0.2) and having differential scanning calorimetric peak at about 189.23 ° C when analyzed at the rate of heating of 10°C per minute and process for preparing the same. A process for resolution of ( S )-1,1'-bi-2-naphthol from RS -1,1'-bi-2-naphthol.
摘要翻译：由（S）-1,1'-联-2-萘酚，3（S） - 叔丁基二甲基甲硅烷基氧化物和（S）-1,1'-联-2-萘酚组成的三元共晶体，（S）-1'-苯基 - 乙基氨基] - 丁酸和3（R） - 丙基-4 - [（S） - 丙基-4 - [（S））具有2θ值为8.41,9.38,10.32,12.16,15.52,15.51,17.84,17.95,19.16,20.37,21.74,22.55,24.44的特征性粉末X射线衍射图的1'-苯基 - 乙基氨基] - 丁酸，25.65,28.40,29.15,29.69,31.31,33.54,34.40,35.43（±0.2），并且在约189.23℃具有差示扫描量热峰。当以每分钟10℃的加热速率进行分析时，以及其制备方法。从RS-1,1'-二-2-萘酚中拆分（S）-1,1'-联-2-萘酚的方法。 >

3. 发明申请

WO2011141923A3 IMPROVED SYNTHESIS OF OPTICALLY PURE (S) - 3-CYANO-5-METHYL-HEXANOIC ACID ALKYL ESTER, AN INTERMEDIATE OF (S)- PREGABALIN 审中-公开
标题翻译：改进的光学纯（S）-3-氰基-5-甲基 - 十六烷酸酸式酯，中间体（S） - 孕酮
公开(公告)号：WO2011141923A3
公开(公告)日：2012-01-19
申请号：PCT/IN2010000440
申请日：2010-06-28
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , PISE VIJAY SADASHIV
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , AGRAWAL MANOJ KUNJABIHARI , PISE VIJAY SADASHIV
IPC分类号： C07C253/30 , C07C51/363 , C07C67/08 , C07C67/343 , C07C231/02 , C07C253/20
CPC分类号： C07C51/363 , C07B2200/07 , C07C67/08 , C07C67/303 , C07C67/343 , C07C253/20 , C07C253/30 , C07C253/34 , C07C255/22 , C07C53/19 , C07C69/40 , C07C69/593 , C07C69/34 , C07C255/19
摘要： The present invention is directed towards synthesis of (S) - 3-cyano-5-methyl-hexanoic acid ethyl ester. A cost effective, eco-friendly process for preparation of enantiomerically pure (S)-3-cyano-5-methyl-hexanoic acid alkyl ester, intermediate of ?-amino acids, particularly (S)-pregabalin.
摘要翻译：本发明涉及（S）-3-氰基-5-甲基 - 己酸乙酯的合成。用于制备对映异构体纯（S）-3-氰基-5-甲基 - 己酸烷基酯的成本有效，环保的方法，α-氨基酸，特别是（S） - 普瑞巴林的中间体。

4. 发明申请

WO2009113081A1 TRIS (HYDROXYMETHYL ) AMINO METHANE SALT OF QUINAPRIL AND RAMIPRIL 审中-公开
标题翻译：奎尼泊尔和RAMIPRIL的TRIS（羟甲基）氨基甲酸盐
公开(公告)号：WO2009113081A1
公开(公告)日：2009-09-17
申请号：PCT/IN2008/000275
申请日：2008-04-28
申请人： LUPIN LIMITED , ROY, Bhairab, Nath , SINGH, Girij, Pal , GODBOLE, Himanshu, Madhav , NEHATE, Sagar, Purushottam , RANANAWARE, Umesh, Babanrao
发明人： ROY, Bhairab, Nath , SINGH, Girij, Pal , GODBOLE, Himanshu, Madhav , NEHATE, Sagar, Purushottam , RANANAWARE, Umesh, Babanrao
IPC分类号： C07D209/52 , C07D217/26
CPC分类号： C07D217/26 , C07D209/52
摘要： The present invention relates to sable tris (hydroxymethyl) amino methane salts of quinapril and ramipril, process for preparation and pharmaceutical formulations thereof.
摘要翻译：本发明涉及喹诺酮和雷米普利的适当的三（羟甲基）氨基甲烷盐，其制备方法和药物制剂。

5. 发明申请

WO2012137142A1 NOVEL SALTS OF RALTEGRAVIR 审中-公开
标题翻译： RALTEGRAVIR的新口号
公开(公告)号：WO2012137142A1
公开(公告)日：2012-10-11
申请号：PCT/IB2012/051651
申请日：2012-04-04
申请人： LUPIN LIMITED , RAY, Purna, Chandra , YADAV, Ashok, Sopanrao , SINGARE, Dnyaneshwar, Tukaram , ARORA, Surinder, Kumar , SINGH, Girij, Pal
发明人： RAY, Purna, Chandra , YADAV, Ashok, Sopanrao , SINGARE, Dnyaneshwar, Tukaram , ARORA, Surinder, Kumar , SINGH, Girij, Pal
IPC分类号： C07D413/12 , A61K31/513 , A61P31/12
CPC分类号： C07D413/12 , A61K31/513 , C07C211/04
摘要： The present invention provides novel salts of raltegravir, viz., meglumine salt, erbumine salt, ammonium salt, tris salt and L-arginine salt of raltegravir and processes for their preparation.
摘要翻译：本发明提供了raltegravir的新型盐，即raltegravir的葡甲胺盐，erbumine盐，铵盐，三盐和L-精氨酸盐及其制备方法。

6. 发明申请

WO2011141805A3 PROCESS FOR THE MANUFACTURE OF LAMIVUDINE 审中-公开
标题翻译：制造拉米夫定的方法
公开(公告)号：WO2011141805A3
公开(公告)日：2012-03-22
申请号：PCT/IB2011001013
申请日：2011-05-12
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , SHRIVASTAVA DHANANJAI , JADHAV HARISHCHANDRA SAMBHAJI , AHER UMESH PARASHRAM , DEOKAR SHARAD CHANDRABHAN
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , SHRIVASTAVA DHANANJAI , JADHAV HARISHCHANDRA SAMBHAJI , AHER UMESH PARASHRAM , DEOKAR SHARAD CHANDRABHAN
IPC分类号： C07D411/04
CPC分类号： C07D411/04
摘要： The present invention relates to an improved process for the Manufacture of Lamivudine. A process for the preparation of essentially enantiomerically pure (-)-[2R, 5S]-4-amino-1-[2- (hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidin-2-one of formula (I), from L-menthyl glyoxylate is described. Also provided is a process for preparation of (+)-1- (2R/S-Cis)-4-amino-1-[(2-hydroxymethyl)-1,3-oxathiolan-5-y1]-2(1H)-pyrimidin-2-one of formula (XII), from L-menthyl glyoxylate.
摘要翻译：本发明涉及拉米夫定的制造方法。制备基本上对映体纯的（ - ） - [2R，5S] -4-氨基-1- [2-（羟甲基）-1,3-氧硫杂环戊烷-5-基] -2（1H） - 嘧啶-2-基 - 描述了式（I）的2-酮，乙醛酸L-薄荷酯。还提供了制备（+） - 1-（2R / S-顺式）-4-氨基-1 - [（2-羟甲基）-1,3-氧硫杂环戊烷-5-基] -2（1H）（XII）的嘧啶-2-酮，由乙醛酸L-薄荷酯。

7. 发明申请

WO2012007814A3 THREE COMPONENT CO-CRYSTAL FORMATION BETWEEN DIASTEREOMERIC MIXTURES OF 3-ALKYL-4-((S)-1'PHENYLETHYLAMINO) BUTANOIC ACID AND OPTICALLY PURE 1, 1'-BI-2-NAPHTHOL 审中-公开
标题翻译： 3-ALKYL-4 - （（S）-1'-苯基氨基甲酸）二油酸和光学纯度1'-BI-2-NAPHTHOL的二元醇混合物之间的三种组分共晶形成
公开(公告)号：WO2012007814A3
公开(公告)日：2012-03-08
申请号：PCT/IB2011001605
申请日：2011-07-11
申请人： LUPIN LTD , ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , MITRA RANGAN
发明人： ROY BHAIRAB NATH , SINGH GIRIJ PAL , LATHI PIYUSH SURESH , MITRA RANGAN
IPC分类号： C07C37/84 , C07C39/14 , C07C229/14
CPC分类号： C07C229/14 , C07B2200/07 , C07B2200/13 , C07C37/84 , C07C39/14
摘要： A ternary co-crystal consisting of 1 :0.5:0.5 molar proportion of (S)-1,1'-bi-2-naphthol, 3(S)-propyl-4-[(S)1 '-phenyl-ethylamino]-butanoic acid and 3(R)-propyl-4-[(S)1'- phenyl-ethylamino]-butanoic acid having characteristic powder X-ray diffraction pattern with 2T values of 8.41, 9.38, 10.32, 12.16, 15.52, 15.51, 17.84, 17.95, 19.16, 20.37, 21.74, 22.55, 24.44, 25.65, 28.40, 29.15, 29.69, 31.31, 33.54, 34.40, 35.43 (±0.2) and having differential scanning calorimetric peak at about 189.23 ° C when analyzed at the rate of heating of 10°C per minute and process for preparing the same. A process for resolution of (S)-1,1'-bi-2-naphthol from RS-1,1'-bi-2-naphthol.
摘要翻译：由（S）-1,1'-双-2-萘酚，3（S） - 丙基-4 - [（S）-1'-苯基 - 乙基氨基] - 丁酸和具有特征性粉末X射线衍射图的3（R） - 丙基-4 - [（S）1'-苯基 - 乙基氨基] - 丁酸，其中2T值为8.41,9.38,10.32,12.16,15.52,15.51 ，17.84,17.95,19.16,20.37,21.74,22.55,24.44,25.65,2840,29.15,29.69,31.31,33.54,34.40,35.43（±0.2），并且当以速率分析时在约189.23℃下具有差示扫描量热峰每分钟加热10℃，其制备方法。从RS-1,1'-双-2-萘酚中分离出（S）-1,1'-双-2-萘酚的方法。

8. 发明申请

WO2010113182A1 INTERMEDIATES IN THE PREPARATION OF 1,4-DIPHENYL AZETIDINONE 审中-公开
标题翻译：制备1,4-二苯基亚甲基二胺的中间体
公开(公告)号：WO2010113182A1
公开(公告)日：2010-10-07
申请号：PCT/IN2010000214
申请日：2010-03-31
申请人： LUPIN LTD , SRIVASTAVA DHANANJAI , SHAKYA RAJIV KUMAR , CHAUDHARI NAMRATA ANIL , ANSARI INAMUS SAQLAIN , SINGH GIRIJ PAL
发明人： SRIVASTAVA DHANANJAI , SHAKYA RAJIV KUMAR , CHAUDHARI NAMRATA ANIL , ANSARI INAMUS SAQLAIN , SINGH GIRIJ PAL
IPC分类号： C07D205/08 , C07D263/22
CPC分类号： C07D263/22 , C07D205/04 , C07D205/08
摘要： The process of the present invention relates to a method for the synthesis of a 1,4-diphenylazetidinone of formula (VIII) by using novel oxime intermediates.
摘要翻译：本发明的方法涉及通过使用新的肟中间体合成式（Ⅷ）的1,4-二苯基氮杂环丁酮的方法。

9. 发明申请

WO2008107911A2 NOVEL PROCESS FOR PREPARATION OF DULOXETINE HYDROCHLORIDE 审中-公开
标题翻译：制备盐酸杜莫西汀的新方法
公开(公告)号：WO2008107911A2
公开(公告)日：2008-09-12
申请号：PCT/IN2008000125
申请日：2008-03-05
申请人： LUPIN LTD , SIYAN RAJINDER SINGH , GOHEL SUNIL KUMAR VINUBHAI , SINGH GIRIJ PAL
发明人： SIYAN RAJINDER SINGH , GOHEL SUNIL KUMAR VINUBHAI , SINGH GIRIJ PAL
IPC分类号： C07D333/20
CPC分类号： C07D333/20
摘要： An improved, safer and easy to operate on plant scale process for synthesis of duloxetine hydrochloride (1) having chiral purity greater than 99.9% that is characterized by the following: (i) preparation of racemic condensed compound (RS)-N,N-di methyl-3- (1-naphthyloxy)-3-(2-thienyl)propanamine (4) by reaction of racemic hydroxy compound (2) with 1-fluronaphthalene (3) in presence of a base such as sodamide, potassium amide or potassium bis(trimethylsilyl)amide (KHDMS) in polar aprotic solvent, (ii) optical resolution of racemic condensed compound (5a + 5b) with di-benzoyl-L-tartaric acid (7, DBTA, R = H) or di-para-anisoyl-L-tartaric acid (7, DATA, R = OCH3) to obtain crude (S)-N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine dibenzoyl tartarate salt (8a) or (S)-N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine di-p-anisoyl tartarate salt (9a) respectively, (iii) optionally purification of crude tartarate salts (8a or 9a) by crystallization, (iv) optionally purification of duloxetine hydrochloride (1) by crystallization and (v) racemization of undesired (R)-N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (5b) by treatment with base potassium bis(trimethylsilyl)amide (KHDMS) to obtain racemic mixture of condensed compounds (5a and 5b). A novel salt S(+)-N.N-dimethyl-3-(1-naphthylenyloxy)-3-(2-thienyl)propanamine dibenzoyl -(L)- tartarate (8a) and S(+)-N.N-dimethyl-3-(1-naphthylenyloxy)-3-(2-thienyl)propanamine di-p-anisoyl-(L)- tartarate (9a). Novel process for racemization of undesired (R)-N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (5b) by treatment with KHDMS to obtain racemic mixture condensed compounds (5a and 5b).
摘要翻译：（1）手性纯度大于99.9％的度洛西汀盐酸盐（1）的合成工艺改进，更安全且易于操作，其特征在于：（i）制备外消旋缩合化合物（RS）-N，通过使外消旋羟基化合物（2）与1-氟萘（3）在碱如氨基磺酸钠，氨基钾或碱土金属的存在下反应，制备2-甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺（二甲基甲硅烷基）氨基钾（KHDMS）在极性非质子溶剂中的溶液，（ii）用二苯甲酰基-L-酒石酸（7，DBTA，R = H）或二（S）-NN-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺二苯甲酰基酒石酸盐（8a）或（S）-N，N-二甲基-3- （S）-NN-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺二 - 对甲氧基苯甲酰基酒石酸盐（9a），（iii）任选纯化粗酒石酸盐（8a或9a）通过结晶，（iv）任选纯化盐酸度洛西汀（1）通过结晶和（v）通过用碱性钾处理不希望的（R）-N，N-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺（三甲基甲硅烷基）酰胺（KHDMS）以获得缩合化合物的外消旋混合物（5a和5b）。（+） - NN-二甲基-3-（1-萘基氧基）-3-（2-噻吩基）丙胺二苯甲酰基 - （L） - 酒石酸盐（8a）和S（+） - NN-二甲基-3- （1-萘基氧基）-3-（2-噻吩基）丙胺二 - 对甲氧基苯甲酰基 - （L） - 酒石酸盐（9a）。用KHDMS处理外消旋不需要的（R）-N，N-二甲基-3-（1-萘氧基）-3-（2-噻吩基）丙胺（5b）的新方法以获得外消旋混合物缩合化合物（5a和5b ）。

10. 发明申请

WO2008053496A2 AN IMPROVED PROCESS FOR THE MANUFACTURE OF LAMIVUDINE 审中-公开
标题翻译：改进的制造方法
公开(公告)号：WO2008053496A2
公开(公告)日：2008-05-08
申请号：PCT/IN2007/000399
申请日：2007-09-10
申请人： LUPIN LIMITED , SINGH, Girij, Pal , SRIVASTAVA, Dhananjai , SATYA, Srinivas, Ayyalasomayajula , SAINI, Manmeet, Brijkishore , JADHAV, Harishchandra, Sambhaji , WARRIER, Aparna, Murlidharan , DUMRE, Nilesh, Bhimsingh
发明人： SINGH, Girij, Pal , SRIVASTAVA, Dhananjai , SATYA, Srinivas, Ayyalasomayajula , SAINI, Manmeet, Brijkishore , JADHAV, Harishchandra, Sambhaji , WARRIER, Aparna, Murlidharan , DUMRE, Nilesh, Bhimsingh
CPC分类号： C07D411/04
摘要： An improved process for the manufacture of Lamivudine. The process involves preparation of racemic cis-(±)-Lamivudine of formula (XII), from a mixture of cis-(±) and trans-(±) intermediate of Formula (IX) by forming a crystalline salt and separating the Cis-(±)-Lamivudine from an organic solvent by fractional crystallization, the said process comprising the steps of: a. providing a mixture of the compound of Formula (IX) and an organic solvent; b. treating the mixture provided in step (a.) with an acid to form its corresponding salt, c. isolating the acid addition salt of the cis-(±) isomers of formula (X), by filtration, d. crystallizing the crude product, e. converting the salt obtained in step (d.) to its free base, f. deprotecting the free base obtained in step (e.) to the compound of Formula (XII). The process for the preparation of an optically pure or optically enriched enantiomer of cis-(-)-Lamivudine of formula (I), from a mixture of racemic cis-(±)-Lamivudine of formula (XII), the said process comprising the steps of: a. providing a mixture of cis-(±)-Lamivudine of Formula (XII) and an organic solvent; the said isomers having the following configurations [2R,5S] and [2S,5R], b. treating the mixture provided in step (a.) with a chiral host, c. isolating the adduct formed by the enantiomer and the chiral host, d. purifying the adduct formed in step (c.) with isopropanol containing a little amount of [S]- BINOL, e. treating the adduct with an acid to form its salt, f. neutralizing this salt using a base, thereby obtaining one of the enantiomers as optically pure Cis-(-)-Lamivudine of formula (I).
摘要翻译：改进的制备拉米夫定的方法。该方法包括通过形成结晶盐从式（IX）的顺式 - （±）和反 - （±）中间体的混合物制备式（XII）的外消旋的顺式 - （±） - 咪达夫定，（±）-Lamivudine通过分级结晶从有机溶剂中提取，所述方法包括以下步骤：a。提供式（IX）化合物和有机溶剂的混合物; 湾用酸处理步骤（a）中提供的混合物以形成其相应的盐，c。通过过滤分离式（X）的顺式（±）异构体的酸加成盐，d。使粗产物结晶，例如，将步骤（d）中获得的盐转化为游离碱，f。将步骤（e）中获得的游离碱脱保护至式（XII）化合物。从式（XII）的外消旋顺式 - （±） - 咪达夫定的混合物制备式（I）的顺式 - （ - ） - 拉米夫定的光学纯的或光学富集的对映异构体的方法，所述方法包括步骤：a。提供式（XII）的顺式 - （±） - 米夫定与有机溶剂的混合物; 所述异构体具有以下构型[2R，5S]和[2S，5R]，b。用手性主体处理步骤（a）中提供的混合物，c。分离由对映异构体和手性主体形成的加合物，d。用含少量[S] - BINOL的异丙醇纯化步骤（c）中形成的加合物，用酸处理加合物以形成其盐，f。使用碱中和该盐，从而获得一种对映异构体作为式（I）的光学纯的顺式 - （ - ） - 拉米夫定。

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